Constrained analogues of procaine as novel small molecule inhibitors of DNA methyltransferase-1.

Castellano, S; Kuck, D; Sala, M; Novellino, E; Lyko, F; Sbardella, G.

doi:10.1021/jm7015705

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Constrained analogues of procaine were synthesized, and their inhibiting activity against DNMT1 was tested. Among them, the most potent compound, derivative 3b, was also able to induce a recognizable demethylation of chromosomal satellite repeats in HL60 human myeloid leukemia cells and thus represents a lead compound for the development of a novel class of non-nucleoside DNMT1 inhibitors.

Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11386/1845456

Titolo:	Constrained analogues of procaine as novel small molecule inhibitors of DNA methyltransferase-1.
Autori interni:	CASTELLANO, Sabrina SBARDELLA, Gianluca SALA, MARINA
Data di pubblicazione:	2008
Rivista:	JOURNAL OF MEDICINAL CHEMISTRY
Abstract:	Constrained analogues of procaine were synthesized, and their inhibiting activity against DNMT1 was tested. Among them, the most potent compound, derivative 3b, was also able to induce a recognizable demethylation of chromosomal satellite repeats in HL60 human myeloid leukemia cells and thus represents a lead compound for the development of a novel class of non-nucleoside DNMT1 inhibitors.
Handle:	http://hdl.handle.net/11386/1845456
Appare nelle tipologie:	1.1.2 Articolo su rivista con ISSN

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